RESUMO
Inflammation is implicated as a cause in many diseases. Most of the anti-inflammatory agents in use are synthetic and there is an unmet need for natural substance-derived anti-inflammatory agents with minimal side effects. Aiouea padiformis belongs to the Lauraceae family and is primarily found in tropical regions. While some members of the Aiouea genus are known to possess anti-inflammatory properties, the anti-inflammatory properties of Aiouea padiformis extract (AP) have not been investigated. In this study, we aimed to examine the anti-inflammatory function of AP through the NOD-, LRR- and pyrin domain-containing protein 3 (NLRP3) inflammasome and elucidate the underlying mechanisms. Treatment with AP inhibited the secretion of interleukin-1 beta (IL-1ß) mediated by NLRP3 inflammasome in J774A.1 and THP-1 cells without affecting the viability. In addition, AP treatment did not influence NF-κB signaling, potassium efflux, or intracellular reactive oxygen species (ROS) production-all of which are associated with NLRP3 inflammasome activation. However, intriguingly, AP treatment significantly reduced the ATPase activity of NLRP3, leading to the inhibition of ASC oligomerization and speck formation. Consistent with cellular experiments, the anti-inflammatory property of AP in vivo was also evaluated using an LPS-induced inflammation model in zebrafish, demonstrating that AP hinders NLRP3 inflammasome activation.
Assuntos
Lauraceae , Proteína 3 que Contém Domínio de Pirina da Família NLR , Animais , Inflamassomos , Peixe-Zebra , Inflamação/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Adenosina Trifosfatases , Extratos Vegetais/farmacologiaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Prostate cancer remains a significant burden in low- and middle-income countries and the second leading cause of death around the world. Spices used in daily cuisine contain interesting phytochemical components capable of helping prevent and cure cancer. AIM: This study aims to give sufficient phytochemical information on two understudied species, Staudtia kamerunensis Warb. (Myristicaceae) and Hypodaphnis zenkeri Engl. Stapf. (Lauraceae), and to study their cytotoxicity against prostate cancer cells in its early form and when they have developed metastasis. MATERIALS AND METHODS: To reach this goal, normal procedures for phytochemical analysis were followed; these include collection, drying, crushing and extraction of plant materials using organic solvents. GC-MS (Gas chromatography- Mass Spectrometry) was used to evaluate the volatile phytochemicals contained in the extracts, and open-column chromatography was used to isolate the pure compounds used in this study. A bio-guided exploration of Hypodaphnis zenkeri (Lauraceae) (leaves, seeds, stems) guided us in selecting the extract for further analysis. An established MTT assay was used to measure cell proliferation. Three prostate cancer cell lines were considered in this study, DU145 and PC3, human androgens-independent prostate carcinoma cells and LNCaP, which are cells derived from metastasis of a human prostate and respond to androgens, oestrogens and progestins. The eight compounds isolated were characterized using HREIMS, 1D and 2D NMR. RESULTS: Among the three extracts from Hypodaphnis zenkeri, considered for biological testing, the leaf extract displayed better activities with a CC50 of 180 µg/mL against DU 145 cells, 184 µg/mL against PC3 cells and 194 µg/mL against LNCaP cells. These results were justified when GC-MS analysis of the different extracts was performed. Fifty compounds were identified from the leaves, representing 96.06% of the volatile components, with most displaying anticancer activities or activities against vectors favorizing cancer growth (inflammation, etc.). An attempt to isolate the active principle responsible for the cancer activity led to the isolation of five pure compounds, namely Eicosane [1], Nonacos-1-ene [2], Palmitic acid [3], Glucoside Stigmasterol [4] and Butane-1,2,3,4-tetraol [5]. Eicosane was identified as being responsible in part for the observed activity, even though it exhibited weak cytotoxicity with the lowest CC50 equal to 30 µg/mL against DU 145 cells. Staudtia kamerunensis sap was investigated in our previous studies with the isolation of Oleanan-12-ene-2α,3ß -diol [6] and 2α, 3ß -dihydroxylup-20-ene [7] among the major components, with significant antibacterial properties. Oleanan-12-ene-2α,3ß -diol [7] in this study displayed a CC50 of 20 µg/mL against DU145 cells, 22 µg/mL against PC3 cells, 18 µg/mL against LNCaP cells, and 32 µg/mL in HMEC affording a selectivity index >2. Contrary to what was observed in our previous study, the activity of Oleanan-12-ene-2α,3ß -diol was lost in the presence of 2α, 3ß -dihydroxylup-20-ene. CONCLUSION: the cytotoxic effect of extract from Staudtia and Hypodaphnis genera and pure isolates are here reported for the first time, as well as the pure isolates. These studies exhibit the cytotoxic potential of two traditional African spices and, more specifically, Oleanan-12-ene-2α,3ß -diol and eicosane, isolated from these plant species.
Assuntos
Antineoplásicos Fitogênicos , Extratos Vegetais , Neoplasias da Próstata , Especiarias , Humanos , Masculino , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/patologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Lauraceae/química , Sobrevivência Celular/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/análise , Cromatografia Gasosa-Espectrometria de Massas , Células PC-3RESUMO
Anti-inflammatory bioassay-guided compound isolation from the exocarp of the Australian rainforest tree Endiandra insignis (family Lauraceae) has led to the discovery and structural elucidation of unusual α, ß-unsaturated twenty-four carbon fatty acids and their positional isomers, insignoic acids A - E (1a - 5c). The stereochemistry and position of the double bond within the aliphatic chain were independently determined via NMR spectroscopy and Ozone-Induced Dissociation (OzID) Mass Spectrometry, respectively. Compounds (1a - 5c) displayed good to moderate anti-inflammatory activity in the range of 8-84 µM. The low therapeutic index observed when assessing the cell viability in the RAW macrophage cell lines, prompted us to investigate the anticancer potential of these unusual fatty acids. The anti-cancer activity was assessed in A-431 carinoma cell lines and MM649 melanoma cell lines. Insignoic acid C (3a-f) exhibited the highest level of potency with an IC50 value of 5-7 µM against both the cell lines. The insignoic acids are the first of their kind known for incorporating an alpha-beta unsaturated system flanked next to a keto group with an additional level of oxygenation at C-6 in a 24carbon fatty acid backbone.
Assuntos
Lauraceae , Árvores , Estrutura Molecular , Floresta Úmida , Austrália , Ácidos Graxos Insaturados , Ácidos Graxos , Anti-Inflamatórios , CarbonoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Litsea glaucescens K. (Lauraceae) is a small tree from the Mexican and Central American temperate forests, named as "Laurel". Its aromatic leaves are ordinarily consumed as condiments, but also are important in Mexican Traditional Medicine, and among the most important non wood forest products in this area. The leaves are currently used in a decoction for the relief of sadness by the Mazahua ethnic group. Interestingly, "Laurel" has a long history. It was named as "Ehecapahtli" (wind medicine) in pre-Columbian times and applied to heal maladies correlated to the Central Nervous System, among them depression, according to botanical texts written in the American Continent almost five centuries ago. AIM OF THE STUDY: Depression is the first cause of incapacity in the world, and society demands alternative treatments, including aromatherapy. We have previously demonstrated the antidepressant-like activity of L. glaucescens leaves' essential oil (LEO), as well as their monoterpenes linalool, and beta-pinene by intraperitoneal route in a mice behavioral model. Here we now examined if LEO and linalool exhibit this property and anxiolytic activity when administered to mice by inhalation. We also investigated if these effects occur by BDNF pathway activation in the brain. MATERIALS AND METHODS: The LEO was prepared by distillation with water steam and analyzed by gas chromatography-mass spectrometry (GC-MS). The monoterpenes linalool, eucalyptol and ß-pinene were identified and quantified. Antidepressant type properties were determined with the Forced Swim Test (FST) on mice previously exposed to LEO or linalool in an inhalation chamber. The spontaneous locomotor activity and the sedative effect were assessed with the Open Field Test (OFT), and the Exploratory Cylinder (EC), respectively. The anxiolytic properties were investigated with the Elevated Plus Maze Apparatus (EPM) and the Hole Board Test (HBT). All experiments were video documented. The mice were subjected to euthanasia, and the brain hippocampus and prefrontal cortex were dissected. RESULTS: The L. glaucescens essential oil (LEO) contains 31 compounds according to GC/MS, including eucalyptol, linalool and beta-pinene. The LEO has anxiolytic effect by inhalation in mice, as well as linalool, and ß-pinene, as indicated by OFT and EC tests. The LEO and imipramine have antidepressant like activity in mice as revealed by the FST; however, linalool and ketamine treatments didn't modify the time of immobility. The BDNF was increased in FST in mice treated with LEO in both areas of the brain as revealed by Western blot; but did not decrease the level of corticosterone in plasma. The OFT indicated that LEO and imipramine didn't reduce the spontaneous motor activity, while linalool and ketamine caused a significant decrease. CONCLUSION: Here we report by the first time that L. glaucescens leaves essential oil has anxiolytic effect by inhalation in mice, as well as linalool, and ß-pinene. This oil also maintains its antidepressant-like activity by this administration way, similarly to the previously determined intraperitoneally. Since inhalation is a common administration route for humans, our results suggest L. glaucescens essential oil deserve future investigation due to its potential application in aromatherapy.
Assuntos
Ansiolíticos , Ketamina , Lauraceae , Litsea , Óleos Voláteis , Humanos , Camundongos , Animais , Ansiolíticos/farmacologia , Ansiolíticos/uso terapêutico , Óleos Voláteis/química , Fator Neurotrófico Derivado do Encéfalo , Imipramina/farmacologia , Eucaliptol/farmacologia , Ketamina/farmacologia , Antidepressivos/farmacologia , Antidepressivos/uso terapêutico , Antidepressivos/química , Monoterpenos/farmacologia , Comportamento AnimalRESUMO
Aniba canelilla (Kunth) Mez essential oil has many biological activities due to its main compound 1-nitro-2-phenylethane (1N2F), followed by methyleugenol, a carcinogenic agent. This study analyzed the influence of seasonality on yields, antioxidant capacity, and 1N2F content of A. canelilla leaf and twig essential oils. Essential oils (EOs) were extracted with hydrodistillation and analyzed with gas chromatography coupled to mass spectrometry and a flame ionization detector. Antioxidant capacity was measured using the free radical scavenging method (DPPH). Chemometric analyses were carried out to verify the influence of climatic factors on the production and composition of EOs. 1-Nitro-2-phenylethane was the major constituent in A. canelilla EOs throughout the seasonal period (68.0-89.9%); methyleugenol was not detected. Essential oil yields and the 1N2F average did not show a statistically significant difference between the dry and rainy seasons in leaves and twigs. Moderate and significant correlations between major compounds and climate factor were observed. The twig oils (36.0 ± 5.9%) a showed greater antioxidant capacity than the leaf oils (20.4 ± 5.0%). The PCA and HCA analyses showed no statistical differences between the oil samples from the dry and rainy seasons. The absence of methyleugenolin in all months of study, described for the first time, makes this specimen a reliable source of 1N2F.
Assuntos
Lauraceae , Óleos Voláteis , Óleos Voláteis/química , Lauraceae/química , Estações do Ano , Antioxidantes/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Folhas de PlantaRESUMO
We examined the niche characteristics and interspecific covariant relationship of main species in Phyllostachys edulis-Alsophila spinulosa association in Chishui A. spinulosa National Nature Reserve under P. edulis disturbance condition, and analyzed the mechanism of competition and coexistence across different species. The results showed that there were 67 species from 53 genera and 40 families in the association. The importance values, Shannon niche breadth index (BS), and Levins niche breadth index (BL) of P. edulis were the largest, indicating its absolute dominant status in association. The importance value and BL of A. spinulosa ranked the second, while BS was the third. There were 190 pairs of 20 main species. The niche overlap between P. edulis and A. spinulosa was the largest, with niche overlap value of 0.64. 71.6% of species pairs had niche overlap of less than 0.2, indicating low niche overlap and high degree of niche differentiation among species. The overall association of main species in association was significantly positive, and the community was relatively stable. The correlation among the main species was not significant, the linkage was not strong, and the species were independent from each other. P. edulis showed significant positive correlation with A. spinulosa, Brassaiopsis glomerulata, Ficus virens, and Mallotus barbatus, while P. edulis showed significant negative correlation with Mallotus philippensis, Cinnamomum glanduliferum, and Machilus gamblei. Niche difference and fitness between P. edulis and natives affected the coexistence and competition among species. Controlling the expansion of P. edulis and limiting the size of species with negative correlation with A. spinulosa could create a favorable living environment for A. spinulosa.
Assuntos
Araliaceae , Lauraceae , Traqueófitas , Humanos , PoaceaeRESUMO
Neocinnamomum delavayi (Lauraceae) leaves with abundant oil cells are seldom attacked by insects, but their chemical constituent and biological function remain obscure. Three furofuran lignans, including (+)-eudesmin (3), (+)-magnolin (4), and demethoxyaschantin (5), were identified to be the major specialized metabolites in the oil cells of N. delavayi leaves through laser microdissection coupled with NMR analysis. Compounds 3 and 4 exhibited obvious antifeedant activity against a generalist insect Spodoptera exigua, and their natural contents in the leaves could effectively defend against generalist insects. Intriguingly, three specific metabolites 9-11, the O-demethylation derivates of compounds 3-5, were identified from a native specialist insect Dindica polyphaenaria feeding with N. delavayi leaves, implying an adaptation mechanism of specialist insects to plant defensive compounds. The results revealed a chemical connection between plants and insects, which would contribute to our understanding of plant-insect interaction and insect management.
Assuntos
Lauraceae , Lignanas , Animais , Insetos , Lignanas/farmacologia , Lignanas/química , SpodopteraRESUMO
The present study aims to explore the anti-inflammatory potential activity of the hexane extract from branches (HEB) of Endlicheria paniculata (Lauraceae) and its main compound, methyldehydrodieugenol B, in the inflammatory response induced by a murine implant sponge model. HPLC-ESI/MS analysis of HEB led to the identification of six chemically related neolignans, with methyldehydrodieugenol B as the main compound. An in silico analysis of the pharmacokinetic parameters of the identified compounds suggested moderate solubility but good absorption and biodistribution in vivo. Thus, the treatment of mice with HEB using in vivo assays indicated that HEB promoted pro-inflammatory, antiangiogenic, and antifibrogenic effects, whereas treatment with methyldehydrodieugenol B caused anti-inflammatory, antifibrogenic, and antiangiogenic effects. The obtained results shown the therapeutic potential of HEB and methyldehydrodieugenol B in the treatment of pathologies associated with inflammation and angiogenesis, including chronic wounds.
Assuntos
Hexanos , Lauraceae , Camundongos , Animais , Distribuição Tecidual , Extratos Vegetais/farmacologia , Inflamação/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Lauraceae/química , Fatores de Transcrição Hélice-Alça-Hélice BásicosRESUMO
Several species of the genus Ocotea are used in traditional medicine due to their anti-inflammatory and analgesic properties. In this work we sought to investigate the effects of biseugenol, the main component of the hexane extract from the leaves of Ocotea cymbarum (Lauraceae), during a chronic inflammatory process induced by polyester-polyurethane sponge in mice. In addition to the inflammatory component, sponge discs also allowed us to evaluate parameters associated with the formation of new blood vessels and the deposition and organization of the extracellular matrix, processes that are related to the chronification of the inflammatory response. Daily treatment with biseugenol (0.1, 1 or 10 µg in 10 µl of 0.5% DMSO) inhibited the synthesis of inflammatory cytokines (TNF-α, CXCL-1 and CCL2) and the neutrophil and macrophage infiltrate into to the implants, indirectly evaluated by the activity of myeloperoxidase and N-acetyl-ß-D-glycosaminidase enzymes, respectively. In implants treated with biseugenol, we observed a reduction in angiogenesis, assessed through histological quantification of mean number of blood vessels, the levels of the pro-angiogenic cytokines FGF and VEGF and the activity of metalloproteinases. Except for VEGF levels, all mentioned parameters showed significant reductions after treatment with biseugenol. Finally, the administration of the compound also reduced TGF-ß1 levels, collagen synthesis and deposition, in addition to modifying the organization of the newly formed matrix, presenting a potential anti-fibrotic effect. Therefore, our results demonstrate the potential therapeutic use of biseugenol for the treatment of a series of pathological conditions, where parameters associated with inflammation, angiogenesis and fibrogenesis are deregulated.
Assuntos
Lauraceae , Ocotea , Animais , Camundongos , Fator A de Crescimento do Endotélio Vascular , Neovascularização Patológica/tratamento farmacológico , Inflamação/tratamento farmacológico , Colágeno , CitocinasRESUMO
Apicomplexan parasites, especially Eimeria sp., are the main intestinal murine pathogens, that lead to severe injuries to farm and domestic animals. Many anticoccidial drugs are available for coccidiosis, which, leads to the development of drug-resistant parasites. Recently, natural products are considered as an alternative agent to control coccidiosis. This study was designed to evaluate the anticoccidial activity of the Persea americana fruit extract (PAFE) in male C57BL/6 mice. A total of 35 male mice were divided into seven equal groups (1, 2, 3, 4, 5, 6, and 7). At day 0, all groups except the first group which served as uninfected-untreated control were infected orally with 1 × 103E. papillata sporulated oocysts. Group 2 served as uninfected-treated control. Group 3 was considered an infected-untreated group. After 60 min of infection, groups 4, 5, and 6 were treated with oral doses of PAFE aqueous methanolic extract (100, 300, and 500 mg/kg of body weight, respectively). Group 7 was treated with amprolium (a reference drug for coccidiosis). PAFE with 500 mg/kg, was the most effective dose, inducing a significant reduction in the output of oocysts in mice feces (by about 85.41%), accompanied by a significant decrease in the number of the developmental parasite stages and a significant elevation of the goblet cells in the jejunal tissues. Upon treatment, a significant change in the oxidative status due to E. papillata infection was observed, where the levels of glutathione (GSH) increased, while, levels of malondialdehyde (MDA) and nitric oxide (NO) were decreased. In addition, the infection significantly upregulated the inflammatory cytokines of interleukin-1ß (IL-1ß), tumor necrosis factor-alpha (TNF-α), and interferon-γ (IFN-γ). This increase in mRNA expression of IL-1ß, TNF-α, and IFN-γ was about 8.3, 10.6, and 4.5-fold, respectively, which significantly downregulated upon treatment. Collectively, P. americana is a promising medicinal plant with anticoccidial, antioxidant, and anti-inflammatory activities and could be used for the treatment of coccidiosis.
Assuntos
Coccidiose , Eimeria , Lauraceae , Persea , Animais , Camundongos , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Fator de Necrose Tumoral alfa , Frutas , Camundongos Endogâmicos C57BL , Coccidiose/tratamento farmacológico , Coccidiose/veterinária , Coccidiose/parasitologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Interferon gama/uso terapêutico , Oocistos , GalinhasRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Aniba canelilla, distributed in the Amazon region, stands out for its diverse economic and medicinal applications. Studies of the A. canelilla essential oil and its primary constituent, 1-nitro-2-phenylethane, have confirmed its anti-inflammatory, antinociceptive, anti-hypertensive potential, and anticholinesterase, among other therapeutic activities. AIM OF THE STUDY: In addition, the present work aims to evaluate the potential of oil and NPE in the learning and memory of rodents. MATERIAL AND METHODS: The oil was hydrodistilled and analyzed by GC and GC-MS. The learning and memory action in mice was evaluated through the scopolamine-induced cognitive deficit model, followed by behavioral analysis using Morris's water maze paradigm. RESULTS: Oil provided a yield of 0.5%, and in its chemical composition, 1-nitro-2-phenylethane (NPE) (76.2%) and methyleugenol (19.6%) were identified as primary constituents. Oil fractionation furnished NPE with 99.4%, which was used to evaluate its effects in animal models. Wistar rats were submitted to the mnemonic impairment-scopolamine-induced protocol for 7 days. The oil, NPE, and the positive control donepezil were administered from the 8th to 12th days. Morris water maze results demonstrated that oil and NPE reversed spatial learning and long-term memory similarly induced by muscarinic antagonist scopolamine to donepezil, the positive control. CONCLUSION: These beneficial effects have led the work to further investigations of the oil and NPE to elucidate their pharmacological mechanism, focusing on the cholinergic pathway of the central nervous system and opening up to the knowledge of other adjacent mechanisms, whose results are still under analysis.
Assuntos
Lauraceae , Óleos Voláteis , Ratos , Camundongos , Animais , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Óleos Voláteis/química , Acetilcolinesterase/metabolismo , Roedores/metabolismo , Ratos Wistar , Donepezila , Lauraceae/química , Escopolamina , Transtornos da Memória/induzido quimicamente , Transtornos da Memória/tratamento farmacológico , Aprendizagem em LabirintoRESUMO
Calmodulin (CaM) and calmodulin-like (CML) proteins are major Ca2+ sensors involved in the regulation of plant development and stress responses by converting Ca2+ signals into appropriate cellular responses. However, characterization and expression analyses of CaM/CML genes in the precious species, Phoebe bournei, remain limited. In this study, five PbCaM and sixty PbCML genes were identified that only had EF-hand motifs with no other functional domains. The phylogenetic tree was clustered into 11 subgroups, including a unique clade of PbCaMs. The PbCaMs were intron-rich with four EF-hand motifs, whereas PbCMLs had two to four EF-hands and were mostly intronless. PbCaMs/CMLs were unevenly distributed across the 12 chromosomes of P. bournei and underwent purifying selection. Fragment duplication was the main driving force for the evolution of the PbCaM/CML gene family. Cis-acting element analysis indicated that PbCaMs/CMLs might be related to hormones, growth and development, and stress response. Expression analysis showed that PbCaMs were generally highly expressed in five different tissues and under drought stress, whereas PbCMLs showed specific expression patterns. The expression levels of 11 candidate PbCaMs/CMLs were responsive to ABA and MeJA, suggesting that these genes might act through multiple signaling pathways. The overexpression of PbCaM3/CML13 genes significantly increased the tolerance of yeast cells to drought stress. The identification and characterization of the CaM/CML gene family in P. bournei laid the foundation for future functional studies of these genes.
Assuntos
Lauraceae , Leucemia Mielogênica Crônica BCR-ABL Positiva , Humanos , Calmodulina/genética , Secas , Filogenia , Cromossomos Humanos Par 12 , Saccharomyces cerevisiaeRESUMO
Abstract Persea lingue Ness is a tree species that lives mainly in temperate forests of south-central Chile. Its leaves are used in ethnomedicine, the fruit is a drupe similar to that of the avocado and has not been studied. The aim of this study was to determine the cytotoxicity in leukemia cell and antibacterial activity, along with some chemical content characteristics of P. lingue fruit and leaf extracts. The antibacterial activity was determined by the inhibition of bacterial growth in liquid medium assay against Gram-positive and Gram-negative bacteria. The leukemia cell lines Kasumi-1 and Jurkat were used to evaluate the cytotoxic activity by using propidium iodide and AlamarBlue assays. Total phenolic, flavonoid, condensed tannin, alkaloid and lipid contents were evaluated in the fruit and in the leaf extracts. The antioxidant activity of both extracts were also elavaluated. Leaf extract presented the highest content of total phenols, condensed tannins and flavonoids, and also the highest antioxidant activity. While the fruit extract has a higher amount of lipids and alkaloids and the high antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus megaterium and Micrococcus luteus. The leaf extract only showed activity against M. luteus. Concerning the cytotoxic activity, only the fruit extract showed cytotoxicity against the cell lines Jurkat and Kasumi-1. P. lingue fruit extract is a potential source of biologically active molecules for the development of new drugs to be used in some types of leukemia, as well as antibacterial agent.
Resumo Persea lingue Ness é uma árvore que vive principalmente na floresta temperada do centro-sul do Chile. As folhas são usadas na etnomedicina. O fruto é uma drupa similar ao abacate e que nunca foi pesquisada anteriormente. O objetivo deste estudo foi o de avaliar a citotoxicidade em células leucêmicas e as atividades antibacterianas, assim como algumas características químicas do extrato de fruto e da folha do P. lingue. As atividades antibacterianas foram determinadas pelo método da inibição do crescimento bacteriano em meio líquido empregando-se bactérias Gram-positivas e Gram-negativas. As linhagens celulares leucêmicas, Kasumi-1 e Jurkat foram usadas para avaliar a atividade citotóxica em ensaios empregando-se iodeto de propídio e AlamarBlue. Foram avaliados os teores totais de fenóis, flavonóides, taninos condensados, alcalóides e lipídeos presentes nos extratos das folhas e dos frutos. As atividades antioxidantes de ambos os extratos também foram avaliadas. O extrato das folhas foi o que apresentou o maior conteúdo de fenóis, taninos condensados e flavonóides totais e a maior atividade antioxidante. Já o extrato de fruto apresentou a maior quantidade de lipídios e alcaloides e a melhor atividade antibacteriana contra Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus megaterium e Micrococcus luteus. Já o extrato das folhas apresentou apenas atividade contra M. luteus. Em relação à atividade citotóxica, apenas o extrato do fruto apresentou citotoxicidade contra as linhagens celulares Jurkat e Kasumi-1. Em resumo, o extrato do fruto de P. lingue é uma potencial fonte de moléculas com atividade biológica para o desenvolvimento de novos fármacos a serem utilizados em alguns tipos de leucemia, bem como agente antibacteriano.
Assuntos
Lauraceae , Persea , Extratos Vegetais/farmacologia , Frutas , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Antibacterianos/farmacologiaRESUMO
Neocinnamomum caudatum (Lauraceae) plant is used in the traditional system of medicine and is considered a potential source of edible fruits, spices, flavoring agents and biodiesel. The leaves, bark and roots of the species are used by local communities for the treatment of inflammatory responses, such as allergies, sinusitis and urinary tract infections. However, there is no scientific evidence to support the molecular mechanism through which this plant exerts its anti-inflammatory effect. The aim of the current research was to characterize the chemical constituents of bark (NCB) and leaf (NCL) essential oil of N. caudatum and to elucidate its anti-inflammatory action in lipopolysaccharide (LPS)-treated RAW 264.7 cells. Essential oils extracted by hydrodistillation were further subjected to gas chromatography mass spectrometry (GC-MS) analysis. The major constituents in bark essential oil identified as ß-pinene (13.11%), α-cadinol (11.18%) and α-pinene (10.99%), whereas leaf essential oil was found to be rich in ß-pinene (45.21%), myrcene (9.97%) and α-pinene (9.27%). Treatment with NCB and NCL at a concentration of 25 µg/mL exerted significant anti-inflammatory activity by significantly reducing LPS-triggered nitric oxide (NO) production to 45.86% and 61.64%, respectively, compared to the LPS-treated group. In the LPS-treated group, the production of proinflammatory cytokines, such as tumor necrosis factor (TNF)-α, interleukin (IL)-6 and IL-1ß, decreased after treatment with essential oil, alleviating the mRNA levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2. The essential oil also inhibited the production of intracellular ROS and attenuated the depletion of mitochondrial membrane potential in a concentration-dependent manner. Pretreatment with NCB also reduced nuclear factor kappa-B (NF-κB)/p65 translocation and elevated the levels of endogenous antioxidant enzymes in LPS-induced macrophages. The present findings, for the first time, demonstrate the anti-inflammatory potential of both bark and leaf essential oils of N. caudatum. The bark essential oil exhibited a significantly more important anti-inflammatory effect than the leaf essential oil and could be used as a potential therapeutic agent for the treatment of inflammatory diseases.
Assuntos
Lauraceae , Óleos Voláteis , Camundongos , Animais , Humanos , NF-kappa B/metabolismo , Lipopolissacarídeos/efeitos adversos , Células RAW 264.7 , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Fator de Necrose Tumoral alfa/metabolismo , Óxido Nítrico , Ciclo-Oxigenase 2/metabolismo , Interleucina-6/metabolismo , Estresse OxidativoRESUMO
Dehydrodieugenol, a neolignan isolated from the Brazilian plant Nectandra leucantha (Lauraceae) with reported antiprotozoal and anticancer activity, was incorporated in Langmuir monolayers of selected lipids as cell membrane models, aiming to comprehend its action mechanism at the molecular level. The interaction of this compound with the lipids dipalmitoylphosphatidylcholine (DPPC), dipalmitoylphosphatidylethanolamine (DPPE), dipalmitoylphosphatidylserine (DPPS), and dipalmitoylphosphatidylglycerol (DPPG) was inferred through tensiometry, infrared spectroscopy, and Brewster angle microscopy. The interactions had different effects depending on the chemical nature of the lipid polar head, with expansion for DPPC monolayers, condensation for DPPE, and expansion (at low surface pressures) followed by the overlap of the isotherms (at high surface pressure values) for DPPS and DPPG. Effects caused by dehydrodieugenol in the negatively charged lipids were distinctive, which was also reflected in the hysteresis assays, surface potential-area isotherms, and rheological measurements. Infrared spectroscopy indicated that the drug interaction with the monolayer affects not only the polar groups, but also the acyl lipid chains for all lipids. These results pointed to the fact that the interaction of the drug with lipid monolayers at the air-water interface is modulated by the lipid composition, mainly considering the polar head of the lipids, as well as the hydrophobicity of the lipids and the drug. As negatively charged lipids pointed to distinctive interaction, we believe this can be related to the antiprotozoal and anticancer properties of the compound.
Assuntos
Lauraceae , Lignanas , Membrana Celular/química , Eugenol/análogos & derivados , Eugenol/análise , Lignanas/análiseRESUMO
Chemical composition and antioxidant activity of the essential oil of Alseodaphne velutina Chev. (Lauraceae) were investigated for the first time from Viet Nam. Leaf essential oil was hydrodistilled and analysed by GC and GC-MS that totally identified 32 terpenoid compounds (accouting for 89.18% of the total oil) with ß-patchoulene (25.74%) and ß-caryophyllene (12.81%) as two major sesquiterpene hydrocarbons compounds. The antioxidant potential of leaf essential oil was evaluated using DPPH, ABTS and FRAP assays, and revealed a moderate-to-high activity comparable with already known antioxidant standard Trolox.
Assuntos
Lauraceae , Óleos Voláteis , Sesquiterpenos , Antioxidantes , VietnãRESUMO
Abstract Essential oils from four Ocotea species collected in southern Brazil were evaluated for chemical composition using gas chromatography coupled with mass spectrometry. The primary compound identified in O. acutifolia essential oil was an unsaturated tetracyclic diterpene, phyllocladene (67.7%), followed by a sesquiterpene hydrocarbon, ß-selinene (18.0%). The sesquiterpene fraction was predominant in oils from two collections of O. puberula; ß-caryophyllene (25.2%) and globulol (22.6%) were the major compounds identified in collections 1 and 2, respectively. O. silvestris essential oil contained predominantly germacrene D and bicyclogermacrene. These compounds were also predominant in essential oil from O. indecora leaves collected from shady habitats. By contrast, essential oil extracted from O. indecora grown under direct sunlight contained mainly oxygenated sesquiterpenes, such as guaiol (30.2%), α-eudesmol (27.6%), and ß-eudesmol (12.7%). Chemotaxis assays showed that Ocotea essential oils had no significant inhibitory activity on leukocyte migration compared with a chemotactic stimulant (lipopolysaccharide from Escherichia coli). However, the oils exhibited antifungal activity against Candida parapsilosis, with a minimum inhibitory concentration of 500 µg/mL. To our knowledge, this is the first study to investigate the in vitro antifungal and antichemotactic activities of essential oils from Ocotea species native to southern Brazil
Assuntos
Óleos Voláteis/química , Ocotea/anatomia & histologia , Produtos Biológicos , Ecossistema , Lauraceae/classificação , Candida parapsilosis , Cromatografia Gasosa-Espectrometria de Massas/métodosRESUMO
Phytochemical analysis of EtOH extract from leaves of Nectandra oppositifolia afforded three flavonoids: kaempferol (1), kaempferol-3-O-α-rhamnopyranoside (2) and kaempferol-3-O-α-(3,4-di-E-p-coumaroyl)-rhamnopyranoside (3), which were characterized by NMR and ESI-HRMS. When tested against the protozoan parasite Trypanosoma cruzi, the etiologic agent of Chagas disease, flavonoids 1 and 3 were effective to kill the trypomastigotes with IC50 values of 32.0 and 6.7 µM, respectively, while flavonoid 2 was inactive. Isolated flavonoids 1-3 were also tested in mammalian fibroblasts and showed CC50 values of 24.8, 48.7 and 153.1 µM, respectively. Chemically, these results suggested that the free aglycone plays an important role in the bioactivity while the presence of p-coumaroyl unities linked in the rhamnoside unity is important to enhance the antitrypanosomal activity and reduce the mammalian cytotoxicity. The mechanism of cellular death was investigated for the most potent flavonoid 3 in the trypomastigotes using fluorescent and luminescent-based assays. It indicated that this compound induced neither permeabilization of the plasma membrane nor depolarization of the membrane electric potential. However, early time incubation (20 min) with flavonoid 3 resulted in a constant elevation of the Ca2+ levels inside the parasite. This effect was followed by a mitochondrial imbalance, leading to a hyperpolarization and depolarization of the mitochondrial membrane potential, with reduction of the ATP levels. During this time, the levels of reactive oxygen species levels (ROS) were unaltered. The leakage of Ca2+ from the intracellular pools can affect the bioenergetics system of T. cruzi, leading to the parasite death. Therefore, flavonoid 3 can be a useful tool for future studies against T. cruzi parasites.
Assuntos
Cálcio/metabolismo , Flavonoides/química , Quempferóis/química , Lauraceae/química , Trypanosoma cruzi/metabolismo , Trifosfato de Adenosina/metabolismo , Animais , Permeabilidade da Membrana Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Feminino , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Íons/química , Lauraceae/metabolismo , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos BALB C , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Trypanosoma cruzi/efeitos dos fármacosRESUMO
Persea lingue Ness is a tree species that lives mainly in temperate forests of south-central Chile. Its leaves are used in ethnomedicine, the fruit is a drupe similar to that of the avocado and has not been studied. The aim of this study was to determine the cytotoxicity in leukemia cell and antibacterial activity, along with some chemical content characteristics of P. lingue fruit and leaf extracts. The antibacterial activity was determined by the inhibition of bacterial growth in liquid medium assay against Gram-positive and Gram-negative bacteria. The leukemia cell lines Kasumi-1 and Jurkat were used to evaluate the cytotoxic activity by using propidium iodide and AlamarBlue assays. Total phenolic, flavonoid, condensed tannin, alkaloid and lipid contents were evaluated in the fruit and in the leaf extracts. The antioxidant activity of both extracts were also elavaluated. Leaf extract presented the highest content of total phenols, condensed tannins and flavonoids, and also the highest antioxidant activity. While the fruit extract has a higher amount of lipids and alkaloids and the high antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus megaterium and Micrococcus luteus. The leaf extract only showed activity against M. luteus. Concerning the cytotoxic activity, only the fruit extract showed cytotoxicity against the cell lines Jurkat and Kasumi-1. P. lingue fruit extract is a potential source of biologically active molecules for the development of new drugs to be used in some types of leukemia, as well as antibacterial agent.
Assuntos
Lauraceae , Persea , Antibacterianos/farmacologia , Frutas , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Extratos Vegetais/farmacologiaRESUMO
Methanolic leaf extracts of four Lauraceae species endemic to Laurisilva forest (Apollonias barbujana, Laurus novocanariensis, Ocotea foetens and Persea indica) were investigated for the first time for their potential to inhibit key enzymes linked to type-2 diabetes (α-amylase, α-glucosidase, aldose reductase) and obesity (pancreatic lipase), and protein glycation. Lauraceae extracts revealed significant inhibitory activities in all assays, altough with different ability between species. In general, P. indica showed the most promissing results. In the protein glycation assay, all analysed extracts displayed a stronger effect than a reference compound: aminoguanidine (AMG). The in vitro anti-diabetic, anti-obesity and anti-glycation activities of analysed extracts showed correlation with their flavonols and flavan-3-ols (in particular, proanthocyanins) contents. These Lauraceae species have the capacity to assist in adjuvant therapy of type-2 diabetes and associated complications, through modulation of the activity of key metabolic enzymes and prevention of advanced glycation end-products (AGEs) formation.